Notwithstanding the physiological hurdles in the gastrointestinal tract, enteral delivery is the most practical route of drug administration. Lipid-based formulations known as nanostructured lipid carriers (NLCs) have received much research as drug-delivery nanovesicles. Due to their superior physical stability, biocompatibility, and enhanced drug-loading capacity, NLCs are preferred over other conventional lipidic nano-formulations, such as liposomes, solid lipid nanoparticles (SLNs), and nanoemulsions. NLCs are considered a promising strategy for oral bioavailability (BAV) enhancement of drugs; this could be due to the benefits of nanomaterials as well as the properties of the lipidic composition of the vesicles, which prevent enzyme degradation, mask unpleasant taste, and being favorably taken up to the lymphatic system through chylomicrons. This review particularly emphasizes their applications as oral drug delivery systems; this review discusses the most recent developments in using NLCs as nanocarriers and their composition, preparation, and characterization techniques.